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CAS No.: 1089283-49-7

GSK1904529A Catalog No. CSN17454

Synonyms: GSK 4529;GSK 1904529;GSK-1904529a

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, being > 100-fold selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述IGF-1R (insulin-like growth factor-1 receptor) plays a key role in transformation, growth and survival of malignant cells, and has been considered as a general and promising target for cancer treatment. GSK1904529A is a selective inhibitor of IGF-IR and IR with IC50 values of 27 and 25nM, respectively. Treatment with GSK1904529A ranging in 0.03-3μM dose-dependently inhibited IGF-1- or insulin-induced autophosphorylation of IGF-1R, as well as the downstream signaling, including phosphorylation of ATK, IRS-1 and ERK. And this inhibition on phosphorylation on IGF-1R and its downstream can be also observed in vivo. In COLO 205, MCF-7, and NCI-H929 cells treated with GSK1904529A ranging in 0.3-10μM for 24h or 48h, dose-dependent increased accumulation in G1 of the cell cycle could be observed. GSK1904529A showed anti-proliferation of cell lines derived from solid and hematologic malignancies, among which multiple myeloma and Ewing's sarcoma cell lines showed most sensitivity. Oral administration of GSK1904529A at 30mg/kg once daily or twice daily for 21 days significantly inhibited tumor growth inhibition of female nude mice bearing tumor xenografts of NIH-3T3/LISN, COLO 205, HT29 and BxPC3, respectively. As GSK1904529A is also a IR inhibitor, minimal effects on blood glucose levels can be observed in animals treated with a single dose of 30 mg/kg GSK1904529A^[1].
作用机制GSK1904529A is a reversible, ATP-competitive inhibitor.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human COLO205 cells	-	Proliferation assay	72 h	Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter assay, IC50=124 nM	19101143
human LP-1 cells	-	Proliferation assay	72 h	Antiproliferative activity against human LP-1 cells after 72 hrs by Celltiter assay, IC50=104 nM	19101143
human NCI-H929 cells	-	Proliferation assay	72 h	Antiproliferative activity against human NCI-H929 cells after 72 hrs by Celltiter assay, IC50=81 nM	19101143

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动物研究
剂量
Mice: 30 mg/kg^[1] (p.o.)

给药途径
p.o.

动物研究
剂量	Mice: 30 mg/kg^[1] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.1738 mL
- 5.8688 mL
- 11.7376 mL
- 5 mM
- 0.2348 mL
- 1.1738 mL
- 2.3475 mL
- 10 mM
- 0.1174 mL
- 0.5869 mL
- 1.1738 mL

技术信息

CAS号

1089283-49-7

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C44H47F2N9O5S

运输

蓝冰

分子量

851.96

别名

GSK 4529;GSK 1904529;GSK-1904529a

溶解度

DMSO	123.0 mg/mL (144.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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